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The biochemical cell culture activities
2022-03-10

The biochemical, cell culture activities and properties of bicyclic carboxamides are compiled in , with the prototype of the series, 4-fluorobenzyl carboxamide , displaying an antiviral profile comparable to the spirocyclic carboxamide . The introduction of a small hydrophobic methyl () and chlori
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The root of Danshen has been widely
2022-03-10

The root of (Danshen) has been widely used as traditional Chinese medicine for many years and shown to exhibit significant pharmacological activities for a variety of human diseases including cancers. Tanshinones, the major active components, belong to a group of an abietane-type diterpenes contain
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H R antagonism can prevent seizure development and
2022-03-10

H3R antagonism can prevent seizure development and improve working memory through the activation of histaminergic neurons (Huang et al., 2004, Zhang et al., 2003). In addition, we have recently found that H3R antagonism protects against ischemia-reperfusion injury via histamine-independent mechanism
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Over recent decades there were three breakthroughs
2022-03-10

Over recent decades, there were three breakthroughs of high intensity heavy-ion acceleration [6]. The first is the invention of radio frequency quadrupole (RFQ) type accelerator, which could accelerate more than dozens of milli-ampere ion beams and is a good solution to space-charge-effect of heavy-
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STAR Methods br Acknowledgments We thank C Hong R Huang
2022-03-10

STAR★Methods Acknowledgments We thank C. Hong, R. Huang, and Z. Yu at the HHMI Janelia cryo-EM facility for help with microscope operation and data collection. We thank A. Müller, W. Kan, and W. Weis for help with the SEC-MALS analysis and M. Elazar and J. Glenn for the use of equipment. P. Love
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br Results and discussion br
2022-03-10

Results and discussion Conclusions A series of novel HDAC inhibitors comprising the thioquinazolinone were designed and synthesized. These derivatives were evaluated for their antiproliferative activities against several human cancer cell lines. Then we chose compounds 7a, 4i, 4o, and 4p to fu
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In addition to understanding the GEF GAP cycle regulating
2022-03-10

In addition to understanding the GEF-GAP cycle regulating Rho-family GTPases, studies have continued to address the role of the Rho-GDIs, which binds to the geranylgeranyl tail to sequester Rho-family GTPases from interacting with lipid membranes, preventing their activation. Whilst it would be temp
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br Introduction Chronic rhinosinusitis with nasal
2022-03-10

Introduction Chronic rhinosinusitis with nasal polyps (CRSwNP), a subgroup of chronic rhinosinusitis (CRS), is a chronic inflammatory condition of the nasal and paranasal sinuses. CRSwNP is characterized by grape-like structures with dense inflammatory infiltrates, loose fibrous sorafenib tosylat
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Selective pharmacological inhibition of tonic currents indic
2022-03-09

Selective pharmacological inhibition of tonic currents indicated that the effects of gp120 are predominantly mediated by α5-containing GABAARs. The other dominant subtype that contributes to tonic current in the hippocampus, the δ-containing GABAAR, was unaffected by gp120 treatment. Additionally, i
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In this study we provide biochemical and immunohistochemical
2022-03-09

In this study we provide biochemical and immunohistochemical evidence for the localization of the glycine transporter GLYT1 in synaptic vesicles. Previously, it was thought that GLYT1 was exclusively a glial protein (Zafra et al., 1995a). However, due to a partial discrepancy between mRNA and protei
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Functional studies based on patch
2022-03-09

Functional studies based on patch-clamp electrophysiology provide additional information on the active state of GlyR α1. Current-voltage measurements from single 78 7 in outside-out patches at symmetric 145-mM chloride concentration yielded a unitary conductance of 86 pS for the main open state and
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br Materials and methods br Results br
2022-03-09

Materials and methods Results Discussion Quercetin is a relatively abundant bioactive flavonoid with a wide variety of documented physiological effects, which has gained popularity as a nutritional supplement [40]. There is increasing interest in quercetin's anticancer properties (for recen
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As glucagon stimulated hepatic glucose production
2022-03-09

As glucagon-stimulated hepatic clobetasol price production is a key component of the normal response to hypoglycemia, the potential of a GCGr antagonist to delay or prevent recovery from a hypoglycemic state is a critical safety issue that must be addressed. Studies of the effects on time to recover
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br Results and discussion br Conclusions As described above
2022-03-09

Results and discussion Conclusions As described above, the SAR study based on compound 1 led to the identification of compound 4 as an ideal inhibitor. An enzyme level investigation showed that 4 is a more potent and selective FGFRs tyrosine kinase inhibitor than is Ponatinib. In addition, the
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ANT located in the IMM mediates the exchange
2022-03-08

ANT, located in the IMM, mediates the exchange of ATP/ADP between the mitochondrial matrix and the intermembrane space (IMS) (Brand et al., 2005; Palmieri and Pierri, 2010). Of the 4 known isoforms, ANT1 is the dominant isoform in the heart (Palmieri and Pierri, 2010). Under physiological conditions
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